Transcription factors are proteins that bind to specific DNA sequences, controlling the transcription of genetic information from DNA to mRNA. Transcription factors play important roles in development, intracellular signaling, and cell cycle, and therefore are of great clinical significance. Many transcription factors are either tumor suppressors or oncogenes, and thus play important roles in cancer development or prevention. Mutations in transcription factors have been associated with specific diseases.
Approximately 10% of currently prescribed drugs directly target transcription factors. Examples include tamoxifen and bicalutamide for the treatment of breast and prostate cancer, respectively, and various types of anti-inflammatory and anabolic steroids. In addition, transcription factors are often indirectly modulated by drugs through signaling cascades. However, most of these treatments are directed at the nuclear receptor class of transcription factors. Other transcription factors outside the nuclear receptor family, such as serum response factor (SRF) transcription factor, are more difficult to target with small molecule therapeutics. Therefore, there is a need for methods of targeting transcription factors that are more difficult to target with small molecule therapeutics, such as serum response factor.